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Vinorelbine Bitartrate lipsome freeze-drying powder injection and its preparation method

A technology of vinorelbine bitartrate and liposome, which is applied in the directions of liposome delivery, freeze-drying delivery, powder delivery, etc., can solve the problems of limited clinical application, large toxic and side effects, etc., and achieve stable drug loading and stability. Good, extended cycle time effect

Inactive Publication Date: 2006-10-04
ZHEJIANG UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, after intravenous injection of the drug, the side effects are relatively large, and the common ones are bone marrow suppression, gastrointestinal toxicity, and hair loss. In addition, long-term use will cause weakness of the lower limbs
These toxic side effects make the clinical application of vinorelbine very limited

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052]Weigh 600mg of soybean lecithin (purity > 76% phosphatidylcholine) and 100mg of cholesterol dissolved in ether, mix well, place the solution in a round bottom flask, and use a rotary evaporator on a constant temperature water bath at 30-32°C Under the condition of 100rpm and reduced pressure, the organic solvent is evaporated, so that the film-forming materials such as phospholipids form a uniform lipid film at the bottom of the flask; 30ml of ether is added to the above-mentioned lipid film to dissolve, and 10mg of vinorelbine is added to 5ml (2- 10ml) in PH7.4 phosphate buffer solution, then it is added in the above-mentioned lipid film solution, rotates and removes organic solvent with rotary evaporator at 32 ℃, until lipid film hydration becomes milky white liposome suspension, Ice bath fractional ultrasound (ultrasonic cell pulverizer) to reduce the particle size. 0.3 mg of vitamin E and 300 mg of mannitol were dissolved in liposomes, and after aseptic filtration (p...

Embodiment 2

[0055] Take by weighing 600mg lecithin (purity>93% phosphatidylcholine) and 100mg cholesterol are dissolved in the 30ml ether; Then vinorelbine is dissolved in the damping fluid of 10mlPH7.4, above-mentioned two liquids are mixed and emulsified, then in 32 Rotate and remove the organic solvent with a rotary evaporator until the mixture turns into a milky white liposome suspension. Ice-bath fractional ultrasound (ultrasonic cell pulverizer) reduces the particle size. 0.3 mg of vitamin E and 300 mg of mannitol were dissolved in liposomes, and after aseptic filtration (pore diameter of membrane filter: 0.2 μm), the final dispersion was divided into vials, and then freeze-dried.

[0056] The vinorelbine liposome preparation of the present invention is a freeze-dried product for injection, and the product quality is stable. The stability experiment was carried out at 25±2°C. The results showed that the product was stable at 25±2°C, and all indicators were within the Within the sco...

Embodiment 3

[0058] Weigh 5 mg of vinorelbine bitartrate, 300 mg of soybean lecithin (purity > 76% phosphatidylcholine) and 30 mg of cholesterol and dissolve them in ether, mix well, place the solution in a ground-mouthed round-bottomed flask, and place it at 30-32°C On a constant temperature water bath, use a rotary evaporator to evaporate the organic solvent under the condition of 100rpm and reduced pressure, so that the film-forming materials such as phospholipids form a uniform lipid film at the bottom of the flask; add 30ml of ether to dissolve the above lipid film, and add 5ml ( 2-10ml) PH7.4 phosphate buffer solution, ultrasonically formed in a water bath, remove the organic solvent with a rotary evaporator at 30°C until it becomes a milky white liposome suspension, and high-pressure emulsify evenly to reduce the particle size. 0.3 mg of vitamin E and 500 mg of mannitol were dissolved in liposomes, and after aseptic filtration (pore diameter of membrane filter: 0.2 μm), the final dis...

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Abstract

The invention relates to an antineoplastic vinorelbine bitartrate liposome, its freeze-dried powder injection and preparing process, wherein the preparation comprises liposome of vinorelbine bitartrate and pharmaceutically acceptable carrying agent, the liposome of vinorelbine bitartrate contains the following constituents: vinorelbine bitartrate, phosphatide, cholesterin and vitamin E, their weight ratio being 1 : 1-100 : 1-15 : 0.01-0.05.

Description

Technical field: [0001] The invention relates to a liposome preparation of antitumor drug vinorelbine bitartrate. Background technique: [0002] Vinorelbine Bitartrate (common name Vinorelbine Bitartrate), is a semi-synthetic vinca alkaloid, its mechanism of action is basically the same as that of vinblastine (VLB) and vincristine (VCR), mainly by blocking The formation of microtubules during cell mitosis stops cell division at metaphase, and is a cell cycle-specific drug. Like other vinblastines, vinorelbine also inhibits amino acid back-and-forth cycling and glutathione metabolism; calmodulin-dependent Ca 甘 -ATPase activity; biological oxidation of cells and biosynthesis of nucleic acids and oils. Clinically, it is mainly used for non-small cell lung cancer, metastatic breast cancer, advanced ovarian cancer, malignant lymphoma, etc. However, after intravenous injection of the drug, the side effects are relatively large, and the common ones are bone marrow suppression, g...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K9/127A61K31/475A61P35/00
Inventor 金一沈圆圆杨雯姝陈长潭王安行
Owner ZHEJIANG UNIV
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